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The abnormal activation of NOD-like receptor protein 3 (NLRP3) inflammasome is related to the development of a variety of inflammatory and autoimmune diseases. In this study, the indole compound A-3 was found to inhibit the activation of the NLRP3 inflammasome pathway. A total of 19 derivatives Ⅰ-1-Ⅰ-4, Ⅱ-1-Ⅱ-6, Ⅲ-1-Ⅲ-3, Ⅳ-1-Ⅳ-6 were synthesized by structural modification of A-3, and 4 compounds Ⅲ-3, Ⅳ-1, Ⅳ-5, Ⅳ-6 could inhibit inflammasome activation at the cellular level. Preliminary mechanistic studies have shown that the compound Ⅳ-5 can inhibit pyroptosis in J774A.1 cell. In addition, we analyzed the structure-activity relationship of the series of compounds based on 3D pharmacophore model. This study provides lead compounds for the development of novel NLRP3 inflammasome pathway inhibitors.
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| 科 Family | 属数 Number of genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) | 属 Genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) |
|---|---|---|---|---|---|---|
| 鹅膏菌科Amanitaceae | 2 | 11 | 5.26 | 鹅膏菌属 Amanita | 10 | 4.78 |
| 小菇科 Mycenaceae | 2 | 12 | 5.74 | 丝盖伞属 Inocybe | 5 | 2.39 |
| 多孔菌科 Polyporaceae | 8 | 14 | 6.70 | 蜡蘑属 Laccaria | 5 | 2.39 |
| 红菇科 Russulaceae | 3 | 23 | 11.00 | 小皮伞属 Marasmius | 6 | 2.87 |
| 小菇属 Mycena | 11 | 5.26 | ||||
| 光柄菇属 Pluteus | 5 | 2.39 | ||||
| 红菇属 Russula | 17 | 8.13 | ||||
| 栓菌属 Trametes | 5 | 2.39 |
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